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EP3077399A4 - Procédés utiles pour la synthèse d'analogues d'halichondrine b - Google Patents

Procédés utiles pour la synthèse d'analogues d'halichondrine b Download PDF

Info

Publication number
EP3077399A4
EP3077399A4 EP14866945.0A EP14866945A EP3077399A4 EP 3077399 A4 EP3077399 A4 EP 3077399A4 EP 14866945 A EP14866945 A EP 14866945A EP 3077399 A4 EP3077399 A4 EP 3077399A4
Authority
EP
European Patent Office
Prior art keywords
halichondrin
analogs
synthesis
methods useful
useful
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP14866945.0A
Other languages
German (de)
English (en)
Other versions
EP3077399A1 (fr
EP3077399B1 (fr
Inventor
Bryan M. Lewis
Yongbo Hu
Huiming Zhang
Hiroyuki Chiba
Yuki Komatsu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eisai R&D Management Co Ltd
Original Assignee
Eisai R&D Management Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Eisai R&D Management Co Ltd filed Critical Eisai R&D Management Co Ltd
Priority to EP18209462.3A priority Critical patent/EP3505520A1/fr
Publication of EP3077399A1 publication Critical patent/EP3077399A1/fr
Publication of EP3077399A4 publication Critical patent/EP3077399A4/fr
Application granted granted Critical
Publication of EP3077399B1 publication Critical patent/EP3077399B1/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/22Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
EP14866945.0A 2013-12-06 2014-12-05 Procédés utiles pour la synthèse d'analogues d'halichondrine b Active EP3077399B1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP18209462.3A EP3505520A1 (fr) 2013-12-06 2014-12-05 Procédés utiles dans la synthèse d'analogues d'halichondrine b

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361912714P 2013-12-06 2013-12-06
PCT/US2014/068834 WO2015085193A1 (fr) 2013-12-06 2014-12-05 Procédés utiles pour la synthèse d'analogues d'halichondrine b

Related Child Applications (2)

Application Number Title Priority Date Filing Date
EP18209462.3A Division-Into EP3505520A1 (fr) 2013-12-06 2014-12-05 Procédés utiles dans la synthèse d'analogues d'halichondrine b
EP18209462.3A Division EP3505520A1 (fr) 2013-12-06 2014-12-05 Procédés utiles dans la synthèse d'analogues d'halichondrine b

Publications (3)

Publication Number Publication Date
EP3077399A1 EP3077399A1 (fr) 2016-10-12
EP3077399A4 true EP3077399A4 (fr) 2017-05-10
EP3077399B1 EP3077399B1 (fr) 2019-02-20

Family

ID=53270478

Family Applications (2)

Application Number Title Priority Date Filing Date
EP18209462.3A Pending EP3505520A1 (fr) 2013-12-06 2014-12-05 Procédés utiles dans la synthèse d'analogues d'halichondrine b
EP14866945.0A Active EP3077399B1 (fr) 2013-12-06 2014-12-05 Procédés utiles pour la synthèse d'analogues d'halichondrine b

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP18209462.3A Pending EP3505520A1 (fr) 2013-12-06 2014-12-05 Procédés utiles dans la synthèse d'analogues d'halichondrine b

Country Status (13)

Country Link
US (4) US9303039B2 (fr)
EP (2) EP3505520A1 (fr)
JP (3) JP6443812B2 (fr)
CN (1) CN105916861B (fr)
BR (1) BR112016012237B1 (fr)
CA (1) CA2931788C (fr)
ES (1) ES2723355T3 (fr)
HU (1) HUE043088T2 (fr)
IL (4) IL245661A0 (fr)
MX (3) MX376869B (fr)
RU (1) RU2676486C1 (fr)
SG (2) SG10201805024YA (fr)
WO (1) WO2015085193A1 (fr)

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EP2522663B1 (fr) 2004-06-03 2015-04-01 Eisai R&D Management Co., Ltd. Intermédiaires pour la préparation d'halichondrine b
RU2489437C2 (ru) 2007-10-03 2013-08-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Промежуточные соединения и способы синтеза аналогов галихондрина в
US8598373B2 (en) 2008-04-04 2013-12-03 Eisai R&D Management Co., Ltd. Halichondrin B analogs
JP5800834B2 (ja) 2010-01-26 2015-10-28 エーザイ・アール・アンド・ディー・マネジメント株式会社 ハリコンドリンb類似体の合成において有用なフロ[3,2−b]ピラン誘導体
CN114716453A (zh) 2013-11-04 2022-07-08 卫材R&D管理有限公司 软海绵素b的类似物合成中有用的大环化反应和中间体
JP6443812B2 (ja) * 2013-12-06 2018-12-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 ハリコンドリンb類縁体の合成に有用な方法
JP2017520586A (ja) 2014-06-30 2017-07-27 プレジデント アンド フェローズ オブ ハーバード カレッジ ハリコンドリン類似体の合成およびその使用
WO2016176560A1 (fr) 2015-04-30 2016-11-03 President And Fellows Of Harvard College Couplage induit par chrome et application à la synthèse d'halichondrines
WO2016179607A1 (fr) 2015-05-07 2016-11-10 Eisai R&D Management Co., Ltd. Réactions de macrocyclisation et intermédiaires et autres fragments utiles dans la synthèse de macrolides halichondrine
MX377663B (es) 2016-02-12 2025-03-11 Eisai R&D Man Co Ltd Intermediarios en la sintesis de eribulina y metodos de sintesis relacionados.
EP3423105B1 (fr) 2016-03-02 2021-05-05 Eisai R&D Management Co., Ltd. Conjugués anticorps-médicament à base d'éribuline et leurs procédés d'utilisation
MX390072B (es) 2016-06-30 2025-03-20 Eisai R&D Man Co Ltd Reaccion de prins e intermediarios utiles en la sintesis de macrolidos de halicondrina y analogos de los mismos.
JP6978758B2 (ja) 2016-11-11 2021-12-08 プレジデント アンド フェローズ オブ ハーバード カレッジ パラジウム媒介ケトール化
HUE060466T2 (hu) 2017-04-05 2023-03-28 Harvard College Makrociklusos vegyület és alkalmazása
US9938288B1 (en) 2017-04-05 2018-04-10 President And Fellows Of Harvard College Macrocyclic compound and uses thereof
WO2018217894A1 (fr) * 2017-05-24 2018-11-29 Eisai R&D Management Co., Ltd. Dérivés d'halichondrine marqués au fluor et procédés de synthèse associés
US11498892B2 (en) 2017-07-06 2022-11-15 President And Fellows Of Harvard College Fe/Cu-mediated ketone synthesis
BR112020000141A2 (pt) 2017-07-06 2020-07-14 President And Fellows Of Harvard College síntese de halicondrinas
CN109694379B (zh) * 2017-10-24 2020-09-11 江苏恒瑞医药股份有限公司 用于制备艾日布林的中间体及其制备方法
ES2974243T3 (es) 2017-11-15 2024-06-26 Harvard College Compuestos macrocíclicos y usos de los mismos
WO2019097073A1 (fr) 2017-11-20 2019-05-23 Basilea Pharmaceutica International AG Associations pharmaceutiques destinées à être utilisées dans le traitement du cancer
CN111868044B (zh) 2018-01-03 2024-07-19 卫材R&D管理有限公司 可用于合成软海绵素大环内酯及其类似物的普林斯反应和化合物
CN112437775A (zh) * 2018-07-20 2021-03-02 雷迪博士实验室有限公司 用于制备艾日布林及其中间体的纯化方法
CN113166096A (zh) * 2018-10-09 2021-07-23 雷迪博士实验室有限公司 制备艾立布林的方法及其中间体
US20220089607A1 (en) * 2018-11-28 2022-03-24 Natco Pharma Limited Process for the preparation of high pure eribulin and its mesylate salt
US11447499B2 (en) 2019-06-14 2022-09-20 Rk Pharma Inc. Process for the preparation of eribulin mesylate intermediate
WO2022101931A1 (fr) * 2020-11-10 2022-05-19 Natco Pharma Limited Procédé de préparation d'éribuline et de ses intermédiaires
CN113354659B (zh) * 2021-06-08 2022-04-08 江苏慧聚药业股份有限公司 甲磺酸艾日布林的合成
CN114380840B (zh) * 2022-01-27 2024-01-26 江苏慧聚药业股份有限公司 艾日布林的合成
WO2025106586A1 (fr) * 2023-11-13 2025-05-22 Luxvitae Therapeutics Inc. Composés cétoniques macrocycliques et leurs applications

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070244187A1 (en) * 2004-06-03 2007-10-18 Eisai Co., Ltd Intermediates for the Preparation of Halichondrin B

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SU652180A1 (ru) 1975-12-16 1979-03-15 Краснодарский политехнический институт 1(Фурил-2,)-2-(2-,, формилфурил-5,, ) этилен или его метильное производное как промежуточный продукт дл синтеза фуран-2,5-дикарбоновой кислоты и способ его получени
US5436238A (en) 1992-03-12 1995-07-25 President And Fellows Of Harvard College Halichondrins and related compounds
US5338865A (en) 1992-03-12 1994-08-16 President And Fellows Of Harvard College Synthesis of halichondrin B and norhalichondrin B
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TW255880B (fr) 1992-09-09 1995-09-01 Hoechst Ag
US6194586B1 (en) * 1996-09-06 2001-02-27 Eli Lilly And Company Selective sulphonation of the primary alcohol of a diol containing both primary and secondary alcohols
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CN109180615A (zh) * 2004-06-03 2019-01-11 卫材R&D管理有限公司 用于制备软海绵素b的类似物的中间体
US20060045846A1 (en) 2004-08-30 2006-03-02 Horstmann Thomas E Reagents and methods for labeling terminal olefins
EP1831697A4 (fr) 2004-12-09 2011-01-26 Eisai R&D Man Co Ltd Criblage de l'isotype tubuline en therapie du cancer faisant appel aux analogues de l'halichondrine b
WO2008010776A1 (fr) 2006-07-21 2008-01-24 Agency For Science, Technology And Research Aigialomycine d et ses dérivés et leur utilisation dans le traitement de cancer ou de paludisme ou d'infection microbienne
JPWO2009014105A1 (ja) 2007-07-20 2010-10-07 株式会社山田養蜂場本社 新規カルボン酸およびそれを有効成分とする抗うつ用組成物
RU2489437C2 (ru) 2007-10-03 2013-08-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Промежуточные соединения и способы синтеза аналогов галихондрина в
CA2705383A1 (fr) 2007-11-16 2009-05-22 Eisai R&D Management Co., Ltd. Nouveau produit intermediaire pour la synthese de l'analogue de l'halichondrine b et nouvelle reaction de desulfonylation utilisee pour le produit intermediaire
US8598373B2 (en) * 2008-04-04 2013-12-03 Eisai R&D Management Co., Ltd. Halichondrin B analogs
JP5371091B2 (ja) 2009-01-23 2013-12-18 三菱レイヨン株式会社 モノスルホン酸エステルの製造方法
JP5800834B2 (ja) 2010-01-26 2015-10-28 エーザイ・アール・アンド・ディー・マネジメント株式会社 ハリコンドリンb類似体の合成において有用なフロ[3,2−b]ピラン誘導体
EP2354128A1 (fr) 2010-02-10 2011-08-10 Sandoz Ag Procédé pour la préparation de rivaroxaban
WO2012147900A1 (fr) 2011-04-28 2012-11-01 Eisai R&D Management Co., Ltd. Procédé en microréacteurs pour synthèse d'analogue d'halichondrine b
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EP2831082B1 (fr) 2012-03-30 2019-02-20 Sandoz AG Procédé de synthèse pour la préparation d'analogues c1-céto macrocycliques de l'halichondrine b et intermédiaires utiles dans celui-ci
CA2916537C (fr) 2013-07-03 2021-07-27 Alphora Research Inc. Procede de synthese pour la preparation d'analogues c1-ceto macrocycliques de l'halichondrine b et intermediaires utiles dans la synthese, notamment des intermediaires contenant d es groupes -so2-(p-tolyle)
CN114716453A (zh) 2013-11-04 2022-07-08 卫材R&D管理有限公司 软海绵素b的类似物合成中有用的大环化反应和中间体
JP6443812B2 (ja) * 2013-12-06 2018-12-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 ハリコンドリンb類縁体の合成に有用な方法
WO2016179607A1 (fr) 2015-05-07 2016-11-10 Eisai R&D Management Co., Ltd. Réactions de macrocyclisation et intermédiaires et autres fragments utiles dans la synthèse de macrolides halichondrine
MX377663B (es) 2016-02-12 2025-03-11 Eisai R&D Man Co Ltd Intermediarios en la sintesis de eribulina y metodos de sintesis relacionados.
MX390072B (es) 2016-06-30 2025-03-20 Eisai R&D Man Co Ltd Reaccion de prins e intermediarios utiles en la sintesis de macrolidos de halicondrina y analogos de los mismos.

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
US20070244187A1 (en) * 2004-06-03 2007-10-18 Eisai Co., Ltd Intermediates for the Preparation of Halichondrin B

Non-Patent Citations (2)

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Title
BRIAN AUSTAD ET AL: "Commercial Manufacture of Halaven : Chemoselective Transformations En Route to Structurally Complex Macrocyclic Ketones", SYNLETT, vol. 24, no. 03, 10 January 2013 (2013-01-10), DE, pages 333 - 337, XP055241626, ISSN: 0936-5214, DOI: 10.1055/s-0032-1318026 *
See also references of WO2015085193A1 *

Also Published As

Publication number Publication date
MX2020004855A (es) 2021-07-08
MX376869B (es) 2025-03-07
BR112016012237A2 (fr) 2017-08-08
WO2015085193A1 (fr) 2015-06-11
US10030032B2 (en) 2018-07-24
US9695188B2 (en) 2017-07-04
US20160176895A1 (en) 2016-06-23
SG10201805024YA (en) 2018-07-30
CN105916861A (zh) 2016-08-31
US20150158881A1 (en) 2015-06-11
IL281275A (en) 2021-04-29
IL245661A0 (en) 2016-06-30
EP3077399A1 (fr) 2016-10-12
US20190010166A1 (en) 2019-01-10
EP3077399B1 (fr) 2019-02-20
MX370611B (es) 2019-12-18
IL273736B (en) 2021-03-25
RU2676486C1 (ru) 2018-12-29
MX2016006891A (es) 2017-06-12
JP2016540752A (ja) 2016-12-28
IL265640A (en) 2019-05-30
JP2019031530A (ja) 2019-02-28
US10450324B2 (en) 2019-10-22
MX2019011926A (es) 2019-11-18
JP2020059739A (ja) 2020-04-16
JP6634135B2 (ja) 2020-01-22
IL273736A (en) 2020-05-31
US20170298078A1 (en) 2017-10-19
IL265640B (en) 2020-04-30
BR112016012237B1 (pt) 2023-02-07
MX384292B (es) 2025-03-14
US9303039B2 (en) 2016-04-05
CA2931788A1 (fr) 2015-06-11
ES2723355T3 (es) 2019-08-26
EP3505520A1 (fr) 2019-07-03
SG11201604545XA (en) 2016-07-28
CA2931788C (fr) 2022-05-24
JP6905041B2 (ja) 2021-07-21
IL281275B (en) 2021-12-01
HUE043088T2 (hu) 2019-08-28
JP6443812B2 (ja) 2018-12-26
CN105916861B (zh) 2018-12-14

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